Pirenzepine

Modify Date: 2024-01-06 12:27:40

Pirenzepine structure	Common Name	Pirenzepine
	CAS Number	28797-61-7	Molecular Weight	351.402
	Density	1.3±0.1 g/cm3	Boiling Point	541.7±50.0 °C at 760 mmHg
	Molecular Formula	C₁₉H₂₃Cl₂N₅O₂	Melting Point	226 - 230ºC
	MSDS	N/A	Flash Point	281.4±30.1 °C

Use of Pirenzepine

Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].

Name	pirenzepine
Synonym	More Synonyms

Description	Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Neuronal Signaling >> mAChR Signaling Pathways >> GPCR/G Protein >> mAChR Research Areas >> Metabolic Disease
In Vitro	Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity[2]. Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration[2]. Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells[2]. Cell Proliferation Assay[2] Cell Line: PC-3 cells Concentration: 100-140 μg/mL Incubation Time: 24 hours Result: Inhibited PC-3 cell proliferation in a concentration-dependent manner. Cell Migration Assay [2] Cell Line: PC-3 and A549 cells Concentration: 110 μg/mL Incubation Time: 24 hours Result: Inhibited the migration of PC-3 and A549 cell lines (P=0.014). Western Blot Analysis[2] Cell Line: PC-3 cells Concentration: 110 μg/mL Incubation Time: 0-24 hours Result: Inhibited the expression of GLI1 and PTCH1. RT-PCR[2] Cell Line: PC-3 cell Concentration: 100-130 μg/mL Incubation Time: 24 hours Result: Suppressed GLI1 mRNA expression in PC-3 cells. Increased PTCH1 mRNA level but not reach statistical significance. Showed no SHH mRNA expression level change.
In Vivo	Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock[3]. Animal Model: Male C57BL/6 mice with experimental endotoxemia[3] Dosage: 0.3 mg/kg Administration: Intraperitoneal injection; 0.3 mg/kg; once Result: Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.

Density	1.3±0.1 g/cm3
Boiling Point	541.7±50.0 °C at 760 mmHg
Melting Point	226 - 230ºC
Molecular Formula	C₁₉H₂₃Cl₂N₅O₂
Molecular Weight	351.402
Flash Point	281.4±30.1 °C
Exact Mass	351.169525
PSA	74.23000
LogP	-0.08
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.615
Storage condition	Store at RT

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UU7882950

CHEMICAL NAME :: 6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-

CAS REGISTRY NUMBER :: 28797-61-7

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H21-N5-O2

MOLECULAR WEIGHT :: 351.45

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3046 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 427 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 156 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,245,1991

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DownStream 0